|Description||A high affinity pan-RAR antagonist (AGN194310, K(d) for binding to RARs = 2-5 nM) inhibited colony formation (by 50%) by all three lines at 16-34 nM, and led to a transient accumulation of flask-cultured cells in G1 followed by apoptosis. AGN194310 is 12-22 fold more potent than all-trans retinoic acid (ATRA) against cell lines and also more potent in inhibiting the growth of primary prostate carcinoma cells. The administration of all-trans retinoic acid to VAD mice resulted in a transient reduction in NF-kappaB activity and, conversely, a single dose of the RAR-pan-antagonist, AGN 194310, administered to control mice, led to a marked, transient induction of whole-body luminescence. Mice were treated with AGN194310, a synthetic retinoid that antagonises the physiological function of the three RAR isotypes (alpha, beta, gamma) but does not interact with RXRs. Analyses of the granulocytic lineage using Gr-1, c-Kit and CD11b antibodies, demonstrated that granulocyte numbers were strikingly increased across haemopoietic compartments in all AGN194310-treated mice. A significant increase in the frequency of progenitor cells containing granulocytes was observed in the bone marrow of mice following treatment with AGN194310.|
|Synonyms||AGN194310; AGN-194310; VTP194310; VTP 194310; VTP-194310|
Adapalene sodium salt
Adapalene sodium salt, a synthetic retinoid, is a Retinoic acid receptor agonist (RAR). It is a third-generation topical retinoid primarily used in the treatmen...
CD 3254 is a selective RXRα agonist with no activity at RARα, RARβ or RARγ receptors.
LE 135 is a retinoic acid antagonist which shows moderate selectivity for RARβ over RARα. It can inhibit human HL-60 leukemia cell differentiation induced by Am...
Adapalene is more active than indomethacin, betamethasone valerate, tretinoin, isotretinoin or etretinate in inhibiting lipoxygease activity, but it has little ...
Acitretin is a second generation retinoid used for psoriasis.
CD 2314 is a potent and selective RARβ receptor agonist (Kd = 145 and >3760 nM for RARβ and RARα receptors, respectively).
AC 261066 is a potent RARβ2 agonist (pEC50 = 8.1).
BMS 195614 is a neutral RAR α-selective antagonist (Ki = 2.5 nM) and exhibits no significant effect on nuclear receptor corepressor (NCoR) binding. BMS 195614 m...